Assay Detail
Binding
CHEMBL4383511
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-Glo assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.47 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439424 | — | — | 1 | 9.70 |
| CHEMBL4519289 | — | — | 1 | 9.70 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 9.00 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439424 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4519289 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1289926 | AXITINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL941 | IMATINIB | IC50 | > | 10000.0 | nM | - |